Cathepsin



Cathepsin (CTS) is a protease which becomes activated at low pH. It is found in lysosomes. Members of the CTS group are denoted as CTSA, CTSB etc and cleave proteins at different peptide bonds. The CTSs are expressed as an inactive precursor pro-CTS (PCTS) which become active when a long residue prosegment is cleaved off producing the mature CTS (MCTS). The images at the left and at the right correspond to one representative Cathepsin, i.e. the crystal structure of wild-type human procathepsin B (1pbh).

3D Structures of Cathepsin
Update June 2011

Procathepsin-B
1pbh, 2pbh, 3pbh – hPCTSB - human

1mir - rPCTSB (mutant) - rat

Cathepsin-B mature
3hhi – TbCTSB (mutant) residues 23-340+CA074 – Trypanosoma brucei

3k9m – hMCTSB+stefin A

3ai8 – hMCTSB + antibiotic

2ipp, 1huc – hMCTSB

3cbj, 3cbk – hMCTSB (mutant)+chagasin

2dc6, 2dc7, 2dc8, 2dc9, 2dca, 2dcb, 2dcc, 2dcd – bMCTSB+inhibitor – bovine

1sp4, 1csb – bMCTSB+epoxysuccinyl inhibitor

1ito, 1qdq – bMCTSB +inhibitor

1gmy - bMCTSB +dipeptidyl nitrile

1the – rMCTSB (mutant)+butanone inhibitor – rat

1cpj - rMCTSB (mutant)

1cte - rMCTSB+pyrimidine inhibitor

Cathepsin-C mature
2djf, 2djg – hMCTSC +Gly-Phe-CHN2

1jqp – rMCTSC

1k3b – hMCTSC

Cathepsin-D mature
1lyw, 1lya – hMCTSD

1lyb - hMCTSD+pepstatin

Cathepsin-E mature
1tzs – hMCTSE+activation peptide from CTSE

Cathepsin-F mature
1m6d – hMCTSF+piperidine inhibitor

Cathepsin-G mature
1kyn – hMCTSG +naphthalene inhibitor

1au8, 1cgh - hMCTSG +phosphonate inhibitor

1t32 - hMCTSG +piperidine inhibitor

Cathepsin-H mature
1nb3, 1nb5 – pMCTSH +stefin A – pig

8pch - pMCTSH

Cathepsin-K mature
3o1g, 3n3g, 2r6n, 1bgo, 3kwz, 3kx1, 3o0u – hMCTSK+ pyrimidine inhibitor

3mpe, 3mpf – hMCTSK (mutant) + pyrimidine inhibitor

3h7d - hMCTSK (mutant) + chondroitin-4-sulfate

3c9e - hMCTSK + chondroitin-4-sulfate

3kwb - hMCTSK (mutant)+dioxo-triazine

3kw9 - hMCTSK +triazine

1yk8 - hMCTSK + cyanamide inhibitor

1yt7 - hMCTSK + ketoamide inhibitor

2aux, 2auz - hMCTSK + semicarbazone inhibitor

1ayu, 1ayv, 1ayw - hMCTSK + carbohydrazide inhibitor

2bdl, 1yk7, 1tu6, 1au3, 1au4 - hMCTSK + pyrrolidine inhibitor

1snk - hMCTSK + norleucine inhibitor

1nl6, 1nlj - hMCTSK+ azepanone inhibitor

1q6k - hMCTSK+carbamate inhibitor

1au0 - hMCTSK+ diacylaminoethyl ketone inhibitor

1au2 - hMCTSK+ propanone inhibitor

1atk – hMCTSK+guanidine inhibitor

1vsn - hMCTSK+ inhibitor

2ato – hMCTSK+myocrisin

1u9v, 1u9x, 1mem – hMCTSK+piperazine inhibitor

1u9w - hMCTSK+imidazole inhibitor

2ftd – MCTSK+azepan inhibitor – Macaca mulatta

2f7d – MCTSK (mutant)+nitrile inhibitor - rabbit

Procathepsin-L
1cjl, 1cs8 - hPCTS-L (mutant)

Cathepsin-L mature
3f75 – MCTSL +CTSL propeptide – Toxoplasma gondii

2p86 – TbMCTSL +K11002

2nqd - CTSL residues 1-220 (mutant)+chagasin – Trypanosoma cruzi

1mhw – hMCTSL +tripeptide

1icf – hMCTSL +MHC class II fragment

Procathepsin-L1
2o6x – hPCTSL1 (mutant) – Fasciola hepatica

Cathepsin-L1 mature
3iv2 – hMCTSL1 (mutant)

3k24 - hMCTSL1 (mutant) +tripeptide

3of8 - hMCTSL1 + dipeptidyl inhibitor

2xu1, 2xu3, 2xu4, 2xu5 - hMCTSL1 catalytic domain (mutant)+nitrile inhibitor

3bc3, 3of9 - hMCTSL1 +inhibitor

3h89, 3h8b, 3h8c - hMCTSL1 (mutant) + retro-binding inhibitor

3hwn, 3hha – hMCTSL1+pyrazole inhibitor

3kse – hMCTSL1 (mutant)+stefin

Cathepsin-L2 mature
3h6s – hMCTSL2+clitocypin

1fh0 – hMCTSL2 (mutant) +vinyl sulfone inhibitor

3kfq - hMCTSL2 (mutant)+stefin

Procathepsin-S
2c0y – hPCTSS (mutant)

Cathepsin-S mature
3n3g, 3n4c - hMCTSS+ pyrimidine inhibitor

3ovx - hMCTSS+ aldehyde inhibitor

3ovz - hMCTSS+ ketoamide inhibitor

3kwn – hMCTSS (mutant)+ thioether acetamide

3iej - hMCTSS (mutant)+pyrazole inhibitor

2h7j, 2hxz- hMCTSS+triazole inhibitor

2r9m, 2r9n, 2r9o – hMCTSS+piperidine inhibitor

2op3, 2hhn, 2g7y, 2hh5, 2f1g – hMCTSS+aryl inhibitor

2fud, 2fra, 2frq, 2ft2, 1npz, 1nqc – hMCTSS+inhibitor

2fye, 2g6d – hMCTSS (mutant)+inhibitor

2fq9, 1ms6 – hMCTSS +nitrile inhibitor

1glo - hMCTSS (mutant)

Procathepsin-X
1deu - hPCTSX

Cathepsin-X mature
1ef7 – hMCTSX